Dopamine - instructions for use, dose, side effects, contraindications

	5 mg / ml	10 mg / ml	20 mg / ml	40 mg / ml
Active substance:
Dopamine hydrochloride	5.0 mg	10.0 mg	20.0 mg	40.0 mg
Auxiliary matter:
Sodium disulfite	1.0 mg	2.0 mg	2.5 mg	5.0 mg
A 0.1 M solution of hydrochloric acid	to pH 2.5-5.0
Water for injections	before 1,0 ml

Description:

Transparent, colorless or slightly yellowish solution.

Pharmacotherapeutic group:cardiotonic agent of non-glycosidic structure

ATX: & nbsp

C.01.C.A.04 Dopamine

Pharmacodynamics:

Excites dopamine, beta-adrenoreceptors (in low and medium doses) and alpha-adrenoreceptors (in high doses). Improvement of systemic hemodynamics leads to a diuretic effect. Has a specific stimulating effect on postsynaptic dopamine receptors in the smooth muscles of blood vessels and kidneys.

In low doses (0.5-3 μg / kg / min) dopamine acts mainly on dopamine receptors, causing the expansion of renal, mesenteric, coronary and cerebral vessels. It has a positive inotropic effect. Expansion of the kidneys leads to increased renal blood flow, increased glomerular filtration rate, increased diuresis and elimination of sodium; There is also an expansion of mesenteric vessels (this effect of dopamine on renal and mesenteric vessels differs from that of other catecholamines).

In medium doses (2-10 μg / kg / min) dopamine stimulates postsynaptic beta₁-adrenoceptors, has a positive inotropic effect (due to increased contractile function of the myocardium) and increases cardiac output.Systolic blood pressure and pulse pressure may increase; the diastolic blood pressure does not change or slightly increases. Coronary blood flow and oxygen consumption of the myocardium, as a rule, increase. Stimulation of beta₂β-adrenoreceptors is negligible or absent, so the total peripheral vascular resistance (OPSS) usually does not change. Peripheral blood flow may decrease slightly, the mesenteric blood flow intensifies.

In high doses (10 μg / kg / min or more) dopamine predominantly stimulates alpha₁-adrenoreceptors, causes an increase in OPSS, an increase in the heart rate and a narrowing of the kidney vessels (the latter can reduce previously increased renal blood flow and diuresis). Due to the increase in the minute volume of blood and OPSS, both systolic and diastolic arterial pressure increase.

The beginning of the therapeutic effect is within 5 minutes against the background of intravenous administration. After stopping the administration, the effect is maintained for 10 minutes. Newborns and young children are more sensitive to the vasoconstrictive effect of dopamine than adults.

Pharmacokinetics:

Dopamine is administered only intravenously. About 25% of the administered dose is captured by neurosecretory vesicles, where hydroxylation occurs and the norepinephrine. It is widely distributed in the body (the volume of distribution in adults is 0.89 l / kg), partially passes through the blood-brain barrier. Communication with blood plasma proteins - 50%.

Dopamine is rapidly metabolized in the liver, kidney and blood plasma by monoamine oxidase and catechol-O-methyltransferase to inactive metabolites of homovanilic acid (HVA) and 3,4-dihydroxyphenylacetate.

Half-life of the drug (T_1/2) - adults: from the blood plasma - 2 min; from the body - 9 minutes; the total clearance of dopamine is 4.4 l / kg / h. It is excreted in the urine; 80% of the dose of dopamine is excreted within 24 hours in the form of metabolites, in small amounts - in unchanged form. In children younger than 2 years, the clearance of dopamine is doubled compared to adults. In newborns there is a significant variability in clearance of dopamine (5-11 minutes, an average of 6.9 minutes). The apparent volume of distribution in newborns is 1.8 l / kg.

Indications:

- Shock of different genesis: cardiogenic, postoperative, infectious-toxic, anaphylactic, hypovolemic (after recovery of the volume of circulating blood);

- acute cardiovascular insufficiency;

- a syndrome of "low minute circulation" in cardiosurgical patients;

- severe arterial hypotension.

Contraindications:

- Hypersensitivity to the components of the drug (including other sympathomimetics);

- thyrotoxicosis;

- pheochromocytoma;

- in combination with monoamine oxidase inhibitors, with cyclopropane and halogen-containing agents for general anesthesia;

- with uncorrected supraventricular and ventricular tachyarrhythmias (including with tachysystolic atrial fibrillation) and with ventricular fibrillation;

- angle-closure glaucoma;

- age to 18 years (efficacy and safety not established).

Carefully:

- Hypovolemia;

- pathological conditions leading to obstruction of the outflow tract of the left ventricle (hypertrophic obstructive cardiomyopathy, marked stenosis of the aortic aorta);

- metabolic acidosis, hypercapnia, hypoxia, hypokalemia;

- diseases of peripheral arteries (including atherosclerosis, arterial thromboembolism, thromboangiitis obliterans,obliterating endarteritis, diabetic angiopathy, Raynaud's disease), frostbite of limbs;

- acute myocardial infarction;

- heart rhythm disturbances;

- arterial hypotension in a small circle of blood circulation;

- diabetes;

- bronchial asthma;

- pregnancy.

Pregnancy and lactation:

Pre-clinical studies have shown that dopamine when administered intravenously at doses up to 6 mg / kg / day, had no teratogenic and fetotoxic effect in rats and rabbits, but increased the mortality of pregnant female rats. The available clinical data are insufficient to assess the fetotoxic and teratogenic effects of dopamine when it is used during pregnancy.

In pregnant women, the drug should be used only if the intended benefit to the mother exceeds the potential risk to the fetus and / or the child.

Data on the penetration of dopamine through the placenta and the excretion of the drug in breast milk are not available. When using Dopamine, breast-feeding should be discontinued.

Dosing and Administration:

Dopamine is administered intravenously drip in the form of continuous infusion with the help of appropriate equipment (infusomats).

The dose of the drug and the rate of administration should be selected individually, depending on the severity of the shock, the magnitude of blood pressure and the patient's response to treatment.

To increase diuresis and achieve a positive inotropic effect (increase in contractile activity of the myocardium) Dopamine is administered at a rate of 100-250 μg / min (1.5-3.5 μg / kg / min - low dose region).

With intensive surgical therapy Dopamine is administered at a rate of 300-700 μg / min (4-10 mkg / kg / min - medium dose area).

With septic shock Dopamine is administered at a rate of 750-1500 μg / min (10.5-20 μg / kg / min - the maximum dose range).

Most patients will be able to maintain a satisfactory condition with Dopamine doses less than 20 μg / kg / min. In some cases, the dose to influence blood pressure of Dopamine may be increased to 40-50 μg / kg / min or more. If the effect of continuous infusion of Dopamine is insufficient, norepinephrine (norepinephrine) in a dose of 5 μg / min (with a patient's body weight of about 70 kg).

If there are or more heart rhythm disturbances, a further increase in the dose of Dopamine is contraindicated.

The duration of dopamine administration depends on the individual characteristics of the patient. There is a positive experience of Dopamine infusion lasting up to 28 days. After stabilization of the patient's condition, the drug is canceled gradually.

The rule of solution preparation: 0.9 dilution is used% solution of sodium chloride, 5% solution of dextrose (glucose) (including mixtures thereof), 5% dextrose (glucose) solution in Ringer's lactate solution, sodium lactate and Ringer's lactate solution.

In order to prepare a solution for intravenous infusion, 400 or 800 mg of dopamine should be added respectively to 250 ml or 500 ml of the above solvents. The resulting solution contains 1600 μg of dopamine in ml.

Preparation of the infusion solution should be performed immediately before use (the stability of the solution remains for 24 hours, except for the mixture with Ringer-lactate solution - maximum 6 hours). The solution of dopamine should be clear and colorless.

Side effects:

Classification of the World Health Organization (WHO) of unwanted drug reactions by frequency of development: very often (> 1/10 appointments); often (> 1/100 and <1/10 of appointments); infrequently (> 1/1000 and <1/100 of prescriptions); rarely (> 1/10000 and <1/1000 appointments); very rarely (<1/10000), including individual messages.

From the cardiovascular system: often - extrasystole, tachycardia, anginal pain, lowering of arterial pressure, symptoms of vasoconstriction. Rarely - bradycardia, conduction disorders, increased blood pressure, expansion of the complex QRS on the ECG; life-threatening ventricular arrhythmias.

From the central nervous system: often - headache; rarely - anxiety, motor anxiety.

From the respiratory system: rarely - shortness of breath.

From the digestive system: often - nausea, vomiting.

From the urinary system: rarely - polyuria (when administered in low doses).

From the side of the organ of vision: rarely - mydriasis.

Reactions at the site of administration: rarely - phlebitis, tenderness at the injection site. If the product gets under your skin - necrosis of the skin and subcutaneous tissue.

Laboratory indicators: rarely - azotemia.

Other: rarely - sawtooth.

Allergic reactions: the drug contains sodium disulfite, the use of which can in rare cases cause or intensify hypersensitivity reactions and bronchospasm (especially in patients with bronchial asthma).

Overdose:

Symptoms: excessive increase of arterial pressure, spasm of peripheral arteries, tachycardia, ventricular extrasystole, angina, shortness of breath, headache, psychomotor agitation.

Treatment: in connection with the rapid excretion of dopamine from the body, these phenomena stop when the dose is reduced or discontinuation of administration. In the case of overdose symptoms, alpha-adrenoblockers are short-acting (with excessive blood pressure increase) and beta-blockers (in case of heart rhythm disturbances).

Interaction:

Pharmaceutical drug interactions

Dopamine is pharmaceutically incompatible with alkaline solutions (inactivate dopamine), Acyclovir, alteplase, amikacin, amphotericin B, ampicillin, cephalothin, dacarbazine citrate, aminophylline (aminophylline), theophylline calcium solution, furosemide, gentamycin, heparin, sodium nitroprusside, benzipenitsillinom, tobramycin, oxidants, iron salts, thiamine (dopamine promotes destruction vitamin A B₁).

Pharmacodynamic drug interactions

With simultaneous use with adrenomimetics,monoamine oxidase inhibitors (including moclobemide, selegiline, furazolidone, procarbazine) and guanethidine, the sympathomimetic effect of dopamine is enhanced (prolongation of duration and enhancement of cardiostimulating and pressor action).

With the simultaneous use of dopamine with diuretics, the diuretic effect of the latter increases.

Inhalation preparations for general anesthesia are hydrocarbon derivatives (cyclopropane, enflurane, halothane, isoflurane, methoxyflurane, chloroform) - increase the cardiotoxic effect of dopamine (increased risk of severe supraventricular or ventricular tachyarrhythmias).

With the simultaneous use of dopamine with tricyclic antidepressants (including maprotiline), selective serotonin reuptake inhibitors and epinephrine (epinephrine) (venlafaxine, milnacipran) and cocaine, pressor effect of dopamine is increased, the risk of heart rhythm disturbances, severe arterial hypertension or hyperpyrexia increases.

With simultaneous use with beta-blockers (propranolol, metoprolol) decrease the pharmacological effects of dopamine.

Butyrophenone derivatives (haloperidol) and phenothiazine reduce the dilatation of mesenteric and renal arteries, caused by low doses of dopamine.

With the simultaneous use of dopamine with guanetidine and preparations containing alkaloids rauwolfia (reserpine, raunatin), severe arterial hypertension may develop. If joint use of these drugs is necessary, the lowest possible doses of dopamine should be used.

With the simultaneous use of dopamine with levodopa, the risk of cardiac rhythm disturbances increases.

With the simultaneous use of dopamine with thyroid hormones, it is possible to increase the pharmacological action of both dopamine and thyroid hormones.

Derivatives of ergot alkaloids (ergometrine, ergotamine, methylergomethrin and others) and oxytocin increase the vasoconstrictor effect of dopamine and increase the risk of ischemia and gangrene, as well as severe arterial hypertension.

Phenytoin with simultaneous application with dopamine can promote the development of arterial hypotension and bradycardia (the effect depends on the dose of the drugs and the rate of administration).

With the simultaneous use of dopamine with cardiac glycosides, inotropic action is intensified and the risk of cardiac rhythm disturbances increases (continuous monitoring of ECG is required).

Dopamine reduces the antianginal effect of nitrates, which, in turn, can reduce the pressor effect of dopamine and increase the risk of arterial hypotension.

Special instructions:

Dopamine is for intravenous infusion only and can only be used in a diluted form!

Before the introduction of Dopamine in patients who are in a state of shock, hypovolemia (through the introduction of blood plasma and other blood substitute fluids), acidosis, hypoxia and hypokalemia should be corrected.

Infusion Dopamine should be administered under the control of diuresis, heart rate, minute blood volume, blood pressure and ECG. Increased blood pressure indicates the need to reduce the dose of Dopamine.

Dopamine improves atrioventricular conduction and can increase the incidence of ventricular contraction in patients with atrial fibrillation and flutter.Dopamine increases the excitability of the myocardium and can lead to the appearance or increase of ventricular extrasystole; the occurrence of ventricular tachycardia and ventricular fibrillation is rare. Patients with a history of such cardiac arrhythmias should continuously monitor the ECG.

Monoamine oxidase inhibitors increase the pressor effect of sympathomimetics and can promote the development of hypertensive crisis and / or heart rhythm disturbances.

Do not use the drug in critically ill patients to correct or prevent acute renal failure.

Strictly controlled studies of the use of the drug in patients under the age of 18 years have not been conducted. There are some reports of the occurrence of arrhythmias and gangrene associated with intravenous drug extravasation in this group of patients.

To reduce the risk of extravasation in patients of any age, dopamine should be injected into large veins whenever possible. To prevent tissue necrosis in case of extravasal ingestion of the drug, a profuse infiltration of the lesion area of 10-15 ml of a 0.9% sodium chloride solution containing 5-10 mg of phentolamine should be immediately performed.The solution is injected with a syringe through a thin needle for subcutaneous injection. Sympathetic blockade of phentolamine leads to the immediate development of local hyperemia within the first 12 hours after exposure to Dopamine, so infiltration should be performed after as short a time as possible after Dopamine extravasation is detected.

When prescribing Dopamine to patients with peripheral vascular disease and / or disseminated intravascular coagulation syndrome (DIC syndrome), an abrupt and pronounced vasoconstriction may occur in the anamnesis, leading to skin necrosis and gangrene of the extremity. Careful monitoring of the patient's condition and circulation in the limbs should be carried out. If there are signs of peripheral ischemia, the drug should be discontinued immediately.

Effect on the ability to drive transp. cf. and fur:

Impact on the ability to drive vehicles or other mechanisms has not been studied.

Form release / dosage:Concentrate for the preparation of a solution for infusions, 5 mg / ml, 10 mg / ml, 20 mg / ml and 40 mg / ml.

Packaging:

5 ml into neutral glass ampoules.

5 ampoules per contour cell pack of polyvinyl chloride film.

1 or 2 contour packs with instructions for use and a vial ampoule or scarifier ampoule in a cardboard box.

5 or 10 ampoules together with the instructions for use and the ampoule ampoule or ampoule ampoule in a pack of cardboard for consumer containers with a corrugated liner.

When using ampoules with a dot or a ring of fracture, the ampoule opener or ampoule scaper is not inserted.

Packing for hospitals

For 50, 100 contour cell packs with ampoules together with an equal number of instructions for use are placed in a box of corrugated cardboard.

Storage conditions:

In the dark place at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003000

Date of registration:21.05.2015

Date of cancellation:2020-05-21

The owner of the registration certificate:ELLARA, LTD. ELLARA, LTD. Russia

Manufacturer: & nbsp

ELLARA, LTD. Russia

Information update date: & nbsp19.01.2016

Illustrated instructions

Instructions

Dopamine (Dofamine)